105

Tofacitinib

105 Publications Verification

Cat. No.: HY-40354

CAS No.: 477600-75-2

Synonyms: Tasocitinib; CP-690550

Target:

JAK STAT NF-κB

Research Areas:

Neurological Disease Metabolic Disease Inflammation/Immunology

Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury .

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105

Tofacitinib citrate

105 Publications Verification

Cat. No.: HY-40354A

CAS No.: 540737-29-9

Synonyms: Tasocitinib citrate; CP-690550 citrate

Target:

JAK STAT NF-κB

Research Areas:

Neurological Disease Metabolic Disease Inflammation/Immunology

Tofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury .

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38

C188-9

38 Cited Publications

Cat. No.: HY-112288

CAS No.: 432001-19-9

Purity: 99.90%

Synonyms: TTI-101

Target:

STAT Apoptosis DNA Methyltransferase

Research Areas:

Metabolic Disease Inflammation/Immunology Cancer

C188-9 (TTI-101) is a STAT3 inhibitor with a K_d value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .

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23

Itacitinib

23 Cited Publications

Cat. No.: HY-16997

CAS No.: 1334298-90-6

Synonyms: INCB039110

Target:

JAK STAT

Research Areas:

Inflammation/Immunology Cancer

Itacitinib (INCB039110) is an orally active selective inhibitor of JAK1 with an IC₅₀ value of 2 nM for human JAK1. Itacitinib inhibits IFN-γ-mediated phosphorylation of STAT1 and downstream pro-inflammatory signaling pathways. Itacitinib reduces the frequency and number of splenic neutrophils in mouse models, downregulates the levels of pro-inflammatory cytokines and chemokines, and inhibits pro-inflammatory gene expression pathways. Itacitinib improves survival rate and clinical scores in mouse models of hemophagocytic lymphohistiocytosis (HLH), and also suppresses metastasis in NSCLC models with high Rab1A expression. Itacitinib can be used for research on hemophagocytic lymphohistiocytosis and non-small cell lung cancer .

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23

Itacitinib adipate

23 Cited Publications

Cat. No.: HY-16997A

CAS No.: 1334302-63-4

Synonyms: INCB039110 adipate

Target:

JAK STAT

Research Areas:

Inflammation/Immunology Cancer

Itacitinib adipate (INCB039110 adipate) is an orally active JAK1-selective inhibitor. Itacitinib adipate inhibits IFN-γ-mediated phosphorylation of STAT1 and downstream pro-inflammatory signaling pathways. Itacitinib adipate reduces the frequency and number of splenic neutrophils in mouse models, downregulates the levels of pro-inflammatory cytokines and chemokines, and inhibits pro-inflammatory gene expression pathways. Itacitinib adipate improves survival rate and clinical scores in mouse models of hemophagocytic lymphohistiocytosis (HLH), and also suppresses metastasis in NSCLC models with high Rab1A expression. Itacitinib adipate can be used for research on hemophagocytic lymphohistiocytosis and non-small cell lung cancer .

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15

Lonafarnib

15 Cited Publications

Cat. No.: HY-15136

CAS No.: 193275-84-2

Purity: 99.60%

Synonyms: Sch66336

Target:

Farnesyl Transferase Tau Protein RSV Akt Ras Bcl-2 Family STAT nAChR Apoptosis Autophagy

Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria .

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12

Abrocitinib

12 Cited Publications

Cat. No.: HY-107429

CAS No.: 1622902-68-4

Purity: 99.26%

Synonyms: PF-04965842

Target:

JAK

Research Areas:

Inflammation/Immunology

Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .

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8

Romaciclib monohydrochloride

8 Cited Publications

Cat. No.: HY-111388A

CAS No.: 2443816-41-7

Purity: 99.29%

Synonyms: SEL120-34A monohydrochloride

Target:

CDK

Research Areas:

Cancer

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 . Has anti-tumor activity .

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